AF 12198 is a peptide that selectively binds Interleukin-1 (IL-1) receptor and blocks in vivo responses to IL-1. The interleukin-1 receptor can activate the innate immune response by binding to cytokines. Dysregulation of cytokine production can lead to aberrant immune cells activation that could result in auto-inflammatory disorders. AF 12198 shows anti-inflammatory activity in vivo.
CAT No: R0918
CAS No:185413-30-3
Synonyms/Alias:AF 12198;185413-30-3;AF12198;Ac-Phe-Glu-Trp-Thr-Pro-Gly-Trp-Tyr-Gln-L-azetidine-2-carbonyl-Tyr-Ala-Leu-Pro-Leu-NH2;DA-60825;FA109195;
AF 12198 is a synthetic peptide compound recognized for its role as a potent and selective antagonist of the melanocortin 4 receptor (MC4R). Characterized by its unique amino acid sequence, AF 12198 interacts specifically with the MC4R, a G protein-coupled receptor implicated in the regulation of energy homeostasis, appetite, and metabolic pathways. Its high receptor affinity and selectivity make it a valuable research tool for elucidating the physiological and biochemical mechanisms underlying melanocortin signaling. As a modulator of peptide-receptor interactions, AF 12198 is widely utilized in advanced studies exploring neuroendocrine function, metabolic regulation, and receptor pharmacology.
Receptor pharmacology: AF 12198 is extensively used in receptor binding assays and functional studies designed to characterize MC4R activity. By competitively inhibiting the binding of endogenous melanocortin peptides, it enables researchers to dissect the specificity and downstream signaling events mediated by MC4R. These investigations are crucial for mapping the pharmacological profile of the receptor, identifying ligand-receptor interactions, and understanding the structural requirements for selective antagonism. The compound's well-defined antagonist properties provide a reliable means to distinguish MC4R-mediated effects from those of related melanocortin receptors.
Metabolic research: In studies of energy balance and metabolic regulation, AF 12198 serves as a molecular tool to explore the role of MC4R in appetite control, energy expenditure, and glucose homeostasis. By blocking MC4R signaling, researchers can investigate the physiological consequences of receptor inhibition, such as alterations in feeding behavior or metabolic rate, within in vitro or ex vivo systems. This application is particularly valuable for delineating the pathways through which melanocortin signaling influences metabolic processes, supporting the development of mechanistic models for energy regulation.
Peptide structure-activity relationship analysis: As a synthetic peptide antagonist, AF 12198 is instrumental in structure-activity relationship (SAR) studies focused on the melanocortin system. Researchers employ the compound to probe how specific amino acid modifications affect receptor binding affinity and selectivity. These SAR investigations provide insights into the molecular determinants of peptide-receptor interactions, guiding the rational design of novel ligands with improved pharmacological profiles. The ability to systematically vary peptide structure while monitoring functional outcomes makes AF 12198 a valuable reference compound in medicinal chemistry and peptide engineering efforts.
Neuroendocrine signaling studies: The compound is frequently applied in neurobiological research to elucidate the role of MC4R in central and peripheral neuroendocrine pathways. By selectively antagonizing MC4R, AF 12198 enables the dissection of signaling networks involved in stress response, hormonal regulation, and neural circuit modulation. These studies often utilize cultured neuronal cells, tissue explants, or biochemical assays to trace the impact of MC4R blockade on neuropeptide release and downstream effector pathways, thereby advancing the understanding of neuroendocrine integration.
Peptide-based assay development: AF 12198 is also employed in the development and optimization of peptide-based assays targeting the melanocortin system. Its defined antagonist activity allows for the calibration of assay sensitivity and specificity, supporting the establishment of robust screening platforms for new MC4R ligands. By serving as a benchmark compound, it facilitates the validation of assay protocols, quality control procedures, and the comparative evaluation of novel peptide or small-molecule antagonists. This application is particularly relevant for laboratories engaged in high-throughput screening or receptor-targeted drug discovery research.
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